半岛bd体育手机客户端 说明
一般描述
The racemic mixture of an aqueous soluble pyridinyl-4H-benzopyran compound that inhibits insulin-regulated aminopeptidase (IRAP) activity by competing against substrate for IRAP extracellular catalytic site binding (Ki= 0.48 ?M against 25 ?M Leu-AMC), while displaying little potency against glucose-6-phosphatase, aminopeptidae N, ACE1, leukotriene A4 hydrolase, or ER-associated aminopeptidases 1 & 2. Reported to boost 1 mM dibutyryl cAMP-evoked glucose uptake in cultured rat hippocampal slices (68% higher uptake with 100 nM HFI-419 than dbcAMP alone)in vitroand exhibitin vivomemory-enhancing efficacay in an object recognition test via direct cerebral lateral ventricle administration (0.1 or 1.0 nmol/2 ?L/rat). HFI-419 is reported to hydrolyze into the less potent HFI-142 (Ki= 2.0 ?M) after i.v. or i.p. injection in rats, although HFI-142 is more stable and likely exhibits better blood-brain permeability.
The racemic mixture of an aqueous soluble (at least 50 ?g/mL or 140 ?M at pH 6.5) pyridinyl-4H-benzopyran compound that inhibits insulin-regulated (IRAP) aminopeptidase activity by competing against substrate for IRAP extracellular catalytic site binding (Ki= 0.48 ?M; using 25 ?M Leu-AMC as substrate) with concomitant interaction with active site zinc via its acetamide, while displaying little potency against glucose-6-phosphatase, aminopeptidase N, ACE1, leukotriene A4 hydrolase, or ER-associated aminopeptidases 1 & 2 (≤13% inhibition at 100 ?M). Reported to boost 1 mM dibutyryl cAMP-evoked glucose uptake in cultured rat hippocampal slices (68% higher uptake in 5 min than dbcAMP alone without 100 nM HFI-419)in vitroand exhibitin vivomemory-enhancing efficacay in an object recognition test when administered directly into the cerebral lateral ventricle of rats via a cannula implant (0.1 or 1.0 nmol/2 ?L/rat). HFI-419 is reported to hydrolyze into slightly less potent HFI-142 (Ki= 2.0 ?M) after i.v. (plasma t1/2= 11 min; 2 mg/kg) or i.p (plasma t1/2= 4.6 h; 10 mg/kg) injection in rats, although HFI-142 is more stable and likely exhibits better blood-brain permeability (Blood:Brain HFI-142 ratio = 3.36 and 0.38, respectively, 0.5 and 4 h post single 3 mg HFI-419/kg i.v. injection).
生化/生理作用
Cell permeable: yes
Primary Target
IRAP
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.
其他说明
Mountford, S.J., et al. 2014.J. Med. Chem.57,1368.
Albiston, A.L., et al. 2011.Br. J. Pharmacol.164,37.
Albiston, A.L., et al. 2010.Mol. Pharmacol.78,600.
Albiston, A.L., et al. 2008.FASEB J.22,4209.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C19H18N2O5 |
| 分子量 | 354.36 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | off-white |
| 溶解性 | DMSO: 100 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
